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Record W4387417568 · doi:10.5267/j.ccl.2023.8.005

Design and synthesis of potential pyrrole-coupled carboxamide derivatives as an anti-superbug MRSA agent

2023· article· en· W4387417568 on OpenAlexvenueno aff
Boobal Arasu Velu, Ganesamoorthy Thirunarayanan, S. Kulanthaivel

Bibliographic record

VenueCurrent Chemistry Letters · 2023
Typearticle
Languageen
FieldChemistry
TopicClick Chemistry and Applications
Canadian institutionsnot available
Fundersnot available
KeywordsChemistryPharmacophoreADMECarboxamideAntibacterial activityCombinatorial chemistryEffluxDocking (animal)Carbon-13 NMRStereochemistryPyrroleMoxifloxacinPharmacologyBacteriaBiochemistryOrganic chemistryAntibioticsIn vitro

Abstract

fetched live from OpenAlex

A series of new pyrrole-coupled carboxamide derivatives had been synthesized and amply characterized by various techniques, viz FTIR, 1H-NMR, 13C-NMR, and LCMS. All these compounds had undergone evaluation for their PASS, BBB, pharmacophore model, ADME, and bioactive score. The antibacterial properties of all the derivatives were examined and compound 5i demonstrated strong antibacterial activity against MRSA. A membrane damage investigation supported by SEM pictures, cellular content leakage, potassium efflux, and bacterial respiration suppression showed that compound 5i had anti-MRSA properties. A good binding score of -9.11 was found for compound 5i against the MRSA protein 6FTB in an in silico molecular docking analysis, compared to a score of -10.25 for streptomycin. Based on these findings, compound 5i can be further studied in order to develop it as a drug to treat MRSA infections.

Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.

How this classification was reachedexpand

Full frame distilled prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.

metaresearch head score (Codex)0.000
metaresearch head score (Gemma)0.000
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesMeta-epidemiology (narrow)
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Bench or experimental · Consensus signal: Bench or experimental
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.003
Threshold uncertainty score1.000

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0000.000
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0000.000
Bibliometrics0.0000.000
Science and technology studies0.0000.000
Scholarly communication0.0000.000
Open science0.0000.000
Research integrity0.0000.000
Insufficient payload (model declined to judge)0.0010.000

Machine scores (provisional)

The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.

Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.

Opus teacher head0.026
GPT teacher head0.271
Teacher spread0.245 · how far apart the two teachers sit on this one work
Validation statusscore_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it

Classification

machine, unvalidated

Machine predicted; a candidate call from one teacher head, not a consensus.

Study designBench or experimental
Domainnot available
GenreEmpirical

How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".

Quick stats

Citations6
Published2023
Admission routes1
Has abstractyes

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